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Modafinil, sold under the brand name Provigil and other brands, is a drug used to treat narcolepsy (English: narcolepsy, also known as narcolepsy, narcolepsy) , Shift work sleep disorder, Drowsiness caused by obstructive sleep apneaOral span>drug.

Modafinil is a prescription drug approved by the U.S. Food and Drug Administration (FDA). Modafinil prescription is required in almost all countries around the world.

Modafinil is not a classic stimulant, but is classified as an arousal-promoting drug. Unlike other stimulants (such as amphetamines), modafinil has minimal peripheral side effects.

Compound summary information

Molecular formula C15H15NO2S

History

Modafinil’s history dates back to the 1970s. It all started with the discovery of a molecule called Adrafinil in the labs of a French pharmaceutical company. Although Adrafinil was originally developed as a potential treatment for narcolepsy, it did not have successful results in early trials. However, a breakthrough came in 1976 when researchers discovered modafinil, Adrafinil's main active metabolite. Unlike its predecessor, Modafinil shows significant effectiveness in promoting wakefulness and increasing the production of key neurotransmitters in the brain. It was quickly recognized by the French military, which used it to increase soldiers' alertness during the Gulf War.

Modafinil was officially registered in France in 1992 and entered the U.S. market under the trade name Provigil in 1998 after being approved by the FDA. Along the way, modafinil gained recognition as a cognitive enhancer, with studies and anecdotal evidence showing its ability to improve memory, concentration, and overall mental acuity. Its safety profile and mild and rare side effects further contribute to its popularity. Recognition from public figures and lifestyle experts has also played an important role in making Modafinil the world's leading smart drug.

Control in different countries

  • United States: Classified as a Schedule IV controlled substance and requires a prescription from a licensed health care provider. It is illegal to import modafinil into the United States.
  • UK: Modafinil is a prescription medicine (POM) used in the UK only to treat narcolepsy , including children (pediatric narcolepsy sleeping sickness). However, possession of modafinil does not constitute a criminal offense as it does not appear in class A, B or C drugs under the UK Misuse of Drugs Act 1971. Importing is legal, but selling is illegal.
  • Australia: Modafinil is a Schedule 4 drug and do not use, buy, sell or possess or attempt to use it unless you have a doctor's prescription for narcolepsy and sleep apnea in Australia. Dafinil is illegal. May be sold under the brand names Modavigil, Modafin, and Nuvigil.
  • Netherlands: Modafinil is only available with a valid narcolepsy doctor's prescription. There is no legal basis to conclude that possession of modafinil is illegal in this country.
  • Germany: Like other Western countries, Modafinil can only be purchased legally in Germany under the brand name "Vigil" by prescription. However, just like in the Netherlands, no laws or regulations can be found stating that possession of modafinil is illegal.
  • Canada: Modafinil is a Schedule 1 prescription drug in Canada, available only by prescription, under the brand name "Alertec". You can't buy it online in the country, but possessing Modafinil is not considered a crime.
  • Mexico: Modafinil can be purchased from any major pharmacy without a prescription and is usually sold under the brand name "Modiodal".
  • Mainland China: Modafinil belongs to the second category of psychotropic drugs.
  • Hong Kong: There are no registered pharmaceutical products containing modafinil or armodafinil in Hong Kong.
  • Taiwan: It is a Class D controlled drug and must be prescribed by a physician to improve the symptoms of excessive daytime sleepiness in patients with narcolepsy.

Mechanism of action

The exact mechanism of action of modafinil is unclear, but in vitro studies have shown that it inhibits dopamine reuptake by binding to dopamine reuptake pumps, resulting in increased extracellular dopamine levels. Additionally, it activates glutamatergic circuits while inhibiting GABA.

It is believed that modafinil may act through a combination of mechanisms, including direct dopamine reuptake inhibition, indirect norepinephrine reuptake inhibition, and orexin activation. It also stimulates α1B-adrenergic receptors.

Adverse reactions and contraindications

Modafinil is contraindicated in people with known hypersensitivity to modafinil or armodafinil. Modafinil is not approved for use in any children, who are at higher risk for rare but serious skin toxicity in these conditions.

Less common serious side effects of Modafinil

  • Black, tarry feces
  • Blurred vision or other vision changes
  • Chest pain
  • Chills or fever
  • Clumsy or unstable
  • Confusion
  • Dizziness or fainting
  • Increased thirst and urination
  • Mental depression
  • Memory problems
  • Rapid changes in mood
  • Shortness of breath
  • Sore throat
  • Shivering or shaking
  • Difficulty urinating
  • Uncontrolled movements of the face, mouth, or tongue
  • Unusual bleeding or bruising
  • Exceptionally tired or weak

Common side effects

  • Anxiety
  • Headache
  • Disgusting
  • Nervous

Severe adverse skin reactions

From 1998 to 2007, the FDA received 6 cases of serious adverse skin reactions related to modafinil, including:

  • Erythema multiforme (EM)
  • Stevens-Johnson Syndrome (SJS)
  • Toxic epidermal necrolysis (TEN)
  • DRESS SYNDROME

Hong Kong Adverse Reaction Report

  • Generalized Tonic-Clonic Seizures (GTCS)
  • Nonconvulsive status epilepticus (NCSE)
  • Visions
  • Autoimmune encephalitis

Addiction and dependence

Modafinil has very low addiction and dependence burden. It shares biochemical mechanisms with addictive stimulants, and some studies report it has similar mood-elevating properties, albeit to a lesser extent. It's unclear whether these effects are more different than those of caffeine. Modafinil does not appear to produce euphoria or abuse in patients at prescribed doses.

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